6533b852fe1ef96bd12aae9c
RESEARCH PRODUCT
In vitro antileishmanial activity of trans-stilbene and terphenyl compounds
Germano CastelliClaudia ColombaManlio TolomeoFederica BrunoFabrizio VitaleMarinella RobertiAntonio CascioLaura GuidottiElisa Giacominisubject
0301 basic medicineMacrophageApoptosisPharmacologychemistry.chemical_compoundStilbenesLeishmania infantumProgrammed cell deathbiologyCell CycleGeneral MedicineU937 CellsFlow CytometryInfectious DiseasesTerphenyl CompoundsLeishmania infantumU937 CellHumanTerphenylLeishmaniasiImmunologyAntiprotozoal AgentsContext (language use)Cercopithecus03 medical and health sciencesInhibitory Concentration 50Structure-Activity RelationshipTerphenylTerphenyl Compoundsparasitic diseasesmedicineStructure–activity relationshipAnimalsHumansAmastigoteLeishmaniasis; Programmed cell death; Stilbenes; Terphenyls; Animals; Antiprotozoal Agents; Apoptosis; Cell Cycle; Cercopithecus; Epithelial Cells; Flow Cytometry; Humans; Inhibitory Concentration 50; Leishmania infantum; Macrophages; Microscopy Fluorescence; Stilbenes; Structure-Activity Relationship; Terphenyl Compounds; U937 Cells; Parasitology; ImmunologyEpithelial CellAnimalCercopithecuMacrophagesTerphenylsApoptosiLeishmaniasisEpithelial CellsTerphenyl Compoundmedicine.diseasebiology.organism_classificationIn vitro030104 developmental biologychemistryMicroscopy FluorescenceStilbeneAntiprotozoal AgentImmunologyParasitologydescription
Leishmaniasis are globally widespread parasitic diseases which often leads to death if left untreated. Currently available drugs present different drawbacks, so there is an urgent need to develop new, safe and cost-effective drugs against leishmaniasis. In this study we tested a small library of trans-stilbene and terphenyl derivatives against promastigote, amastigotes and intramacrophage amastigote forms of Leishmania infantum. Two compounds of the series, the trans-stilbene 3 and the terphenyl 11, presented the best activity and safety profiles. Terphenyl 11 showed a leshmanicidal activity higher than pentostam and the ability to induce apoptosis selectively in Leishmania infantum while saving macrophages and primary epithelial cells. Our data indicate that terphenyl compounds, as well as stilbenes, are endowed with leishmanicidal activity, showing potential for further studies in the context of leishmanial therapy.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2016-07-01 |